Journal of Pharmaceutical Sciences p. 1214 - 1219 (1982)
Update date:2022-07-30
Topics:
Crider
Tita
Wood
Hinko
A variety of esters of nipecotic and isonipecotic acids were synthesized and evaluated for anticonvulsant activity. The ester group was varied in terms of lipophilicity and reactivity toward hydrolysis. The esters were screened against seizures induced by electroshock, pentylenetetrazol, and the putative γ-aminobutyric acid antagonist, bicuculline. The most significant activity was demonstrated by the p-nitrophenyl esters of nipecotic and isonipecotic acids against bicuculline-induced seizures. Esters of nipecotic acid were tested for in vitro inhibition of γ-aminobutyric acid and L-proline uptakes into mouse whole brain minislices. The p-nitrophenyl, n-octyl, and succinimidyl esters were the most potent inhibitors of γ-aminobutyric acid uptake. The uptake of γ-aminobutyric acid by the ester derivatives appeared to involve specific and nonspecific mechanisms.
View Morewebsite:http://www.konochem.com
Contact:86-29-86107037-8015
Address:No.11 Daqing Road,Lianhu District,Xi’an 710082,China
shanghai jiuling chemical co.,ltd.
Contact:+86-21-50387295
Address:Zaozhuang Road, Pudong, Shanghai City. China
Kaiping Genuine Biochemical Pharmaceutical Co.,Ltd.
Contact:+86-750-2881198
Address:No.1, Xinke Road, Shatang Town, Kaiping, Guangdong Province, P.R.China
Contact:+86-13914766747
Address:Floors 21&22, Jin Cheng Tower, No. 216 Middle Longpan Road, Nanjing
Contact:+8613400661290
Address:No 908,Kangwan Rd, Liuyang Economic
Doi:10.1021/acs.joc.0c02696
(2021)Doi:10.1016/j.tet.2004.11.026
(2005)Doi:10.1055/s-1982-29910
(1982)Doi:10.1248/cpb.30.3457
(1982)Doi:10.1002/jhet.5570410620
(2004)Doi:10.1002/ejoc.200500296
(2005)